α‐Fluorotricarbonyl Derivatives as Versatile Fluorinated Building Blocks: Synthesis of Fluoroacetophenone, Fluoroketo Ester and Fluoropyran‐4‐one Derivatives

Abstract

Fluorinated acyl‐Meldrum's acid derivatives were synthesized by electrophilic fluorination of appropriate phenacyl Meldrum's acid substrates using Selectfluor. Reactions with water, ethanol, Grignard, and alkynyllithium reagents gave rise to the corresponding fluoro‐acetophenone, –1,3‐keto ester, –1,3‐diketone and ‐pyran‐4‐one products respectively from the same selectively fluorinated scaffold in one‐step procedures.

Initial Route Scouting and Final Process Development for the Multi-Kg Production of 3-Fluoro-6-methoxyquinoline from p-Anisidine and 2-Fluoromalonic Acid

“…The reaction was dose-controlled and >98% conversion to fluorinated 2-acyl malonate 19 was routinely observed after addition. To the best of our knowledge, this is the first reported fluorination of such an acylated malonate system as 4 . The reaction mixture was quenched with 20% aq citric acid.…”

Discovery of 4-nitro-3-phenylisoxazole derivatives as potent antibacterial agents derived from the studies of [3 + 2] cycloaddition

“…1 ) was developed and applied to control the plant pathogens in crops such as rice, citrus, and kiwi fruit. 6 Bismerthiazol ( Fig. 1 ) was used to control the effect of rice bacterial blight and bacterial leaf streak.…”